Lurasidone - CAS 367514-87-2
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Not Intended for Therapeutic Use. For research use only.
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Lurasidone is a new atypical antipsychotic developed by Dainippon Sumitomo Pharma and marketed by Sunovion in the USA. In the USA, it is also approved for the treatment of depressive episodes associated with bipolar I disorder (bipolar depression) in adults when used alone or in combination with lithium or valproate. It acts as a dopamine D2 receptor antagonist.
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Brife Description:
atypical antipsychotic, depressive episodes
Latuda; Lurasidone hydrochloride; UNII-22IC88528T; SM-13496
atypical antipsychotic, the treatment of depressive episodes associated with bipolar I disorder
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1. Determination of dopamine D2 receptor occupancy by lurasidone using positron emission tomography in healthy male subjects
Dean F. Wong & Hiroto Kuwabara. Psychopharmacology (2013) 229:245–252
Lurasidone is rapidly absorbed following oral administration, with peak serum concentration achieved within 1–3h of dosing (Ehret et al. 2010;Citrome 2011; Latuda USPI 2012). Lurasidone is primarily metabolized by CYP3A4, yielding two active metabolites accounting for 24 % (ID-14283) and 3 % (ID-14326) of parent compound exposure. There is a linear relationship between dose and serum concentration of lurasidone in the dosing range of 20–160 mg (Latuda USPI 2012). The mean serum elimination half-life of the parent compound is approximately 18 h (Citrome 2011;Latuda USPI 2012). Unlike amisulpride, aripiprazole, olanzapine, and risperidone (Moons et al. 2011), neither lurasidone nor its active metabolite (ID-14283) are substrates for P-glycoprotein (Meyer et al. 2009).
2. A Sensitive and Selective LC-MS Method for the Determination of Lurasidone in Rat Plasma, Bile, and Urine
Yoon-Jee Chae • Tae-Sung Koo • Kyeong-Ryoon Lee. Chromatographia (2012) 75:1117–1128
Through its action on these different receptors, lurasidone has a better tolerability than the other antipsychotic drugs, with less weight gain (H1 receptor), less risk of orthostatic hypertension (α2C and α1 receptors), less sedative effects (H1 and M1 receptors), and less anticholinergic effects (M1 receptors). In addition, lurasidone has been reported to be superior to other antipsychotics in reversing dizocilpine (MK-801)-induced learning and memory impairment. Collectively, the drug may be clinically useful for the treatment of schizophrenia with less adverse effects.
3. Lurasidone in Schizophrenia: New Information About Dosage and Place in Therapy
Leslie Citrome. Adv Ther (2012) 29(10):815–825.
Similar to most other second-generation antipsychotics, lurasidone is a full antagonist at dopamine D2 and serotonin 5HT2A receptors. However, lurasidone also has high affinity for serotonin 5HT7 receptors (comparable to dopamine D2 and 5HT2A receptors) and is a partial agonist at 5HT1A receptors. Lurasidone has moderate affinity for alpha 2C noradrenergic receptors. Differences among antipsychotics in these and other binding characteristics may offer an explanation for the heterogeneity of effects observed between drugs and among different patients.
4. Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals
Sunny Shah, Bhavin Parmar, Moinuddin Soniwala, and Jayant Chavda. AAPS PharmSciTech
Lurasidone hydrochloride (3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl) piperazin-1-ylmethyl] cyclohexylmethyl} hexahydro-4,7-methano-2H isoindole-1,3-dione hydrochloride (Fig. 1) is an atypical antipsychotic and mediates its pharmacological action by blocking central dopamine D2 neuroreceptors. Lurasidone hydrochloride has been approved by the US Food and Drug administration for treatment of bipolar depression alone or in combination with lithium in adults. It is currently marketed under the trade name of LatudaTM and is a drug of choice since it causes minimal effects on body weight, has low potential of sedation, and does not cause significant changes across metabolic parameters. The innovator concludes that lurasidone absorption is influenced by food consumption and when administered with food the absorption of lurasidone showed a twofold increase; the maximum concentration (Cmax) also increased by threefold. The Tmax is shown to increase by 0.5–1.5 h with food. Considering the significant food effect on the bioavailability of lurasidone, it is recommended to be administered once daily with at least 350 cal of food.
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CAS 367514-87-2 Lurasidone

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